α1-Adrenergic receptors: New insights and directions

Michael T. Piascik, Dianne M. Perez

Research output: Contribution to journalReview articlepeer-review

325 Scopus citations

Abstract

The adrenergic receptors play a key role in the modulation of sympathetic nervous system activity as well as a site of action for many therapeutic agents. The α1-adrenergic receptor subtypes (α1A-, α1B-, α1D) are the prime mediators of smooth muscle contraction and hypertrophic growth, but their characterization in both binding and function have lagged the other adrenergic family members. Although they are derived from a related ancestral gene and all nine adrenergic receptor family members bind the endogenous ligands, epinephrine and norepinephrine, with roughly similar affinities, there are major differences in the mode of binding, second messenger utilization, and physiological effects of the α1-subtypes compared with β-or α2-subtypes. Here, we review the recent literature on aspects of its binding pocket and how it differs from the β-adrenergic receptor paradigms. We also review the signaling components and aspects of its function and provide new insights into its roles in smooth muscle, growth, neurological, and cardiovascular function.

Original languageEnglish
Pages (from-to)403-410
Number of pages8
JournalJournal of Pharmacology and Experimental Therapeutics
Volume298
Issue number2
StatePublished - 2001

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmacology

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